US10941116B2ActiveUtilityA1

Crystalline forms of mesaconine and preparation methods therefor

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Assignee: GOODDOCTOR PHARMACEUTICAL GROUP CO LTDPriority: Jan 24, 2018Filed: Jan 23, 2019Granted: Mar 9, 2021
Est. expiryJan 24, 2038(~11.5 yrs left)· nominal 20-yr term from priority
A61P 9/04C07D 471/08C07D 221/22C07B 2200/13A61K 31/439
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PatentIndex Score
1
Cited by
16
References
6
Claims

Abstract

The present invention relates to crystalline forms of mesaconine. Specifically, the present invention relates to crystalline form A, crystalline form B and crystalline form C of mesaconine and preparation methods thereof. In the method, the mesaconine is crystallized in solvent, and then the crude crystal is dried to obtain target crystalline form. The crystalline forms of mesaconine according to the present invention have good solubility, good stability, low hygroscopicity, long-term storage capability and good reproducibility, and have a good prospect to be developed as pharmaceuticals.

Claims

exact text as granted — not AI-modified
The invention claimed is: 
     
       1. Crystalline form A of mesaconine, wherein, the crystalline form A of mesaconine exhibits characteristic peaks at 2θ of 8.3°±0.2°, 10.6°±0.2°, 13.3°±0.2°, 13.7°±0.2° and 19.0°±0.2° in powder X-ray diffraction spectrum using Cu-Kα radiation. 
     
     
       2. The crystalline form A of mesaconine according to  claim 1 , wherein, the crystalline form A of mesaconine also exhibits characteristic peaks at 2θ of 11.6°±0.2°, 19.8°±0.2°, 24.2°±0.2° and 26.9°±0.2° in powder X-ray diffraction spectrum using Cu-Kα radiation. 
     
     
       3. A method for preparing the crystalline form A of mesaconine according to  claim 1 , wherein, the method comprises steps of:
 (1) adding mesaconine into a solvent, then heating the obtained solution to 50˜90° C. to dissolve the mesaconine so as to obtain a mesaconine solution; 
 (2) cooling the mesaconine solution to −10˜30° C., stirring the solution to precipitate crystal, and then performing filtration; 
 (3) drying the solid obtained by filtration in the step (2) at vacuum to obtain the crystalline form A of mesaconine. 
 
     
     
       4. The method according to  claim 3 , wherein, the solvent is selected from a group consisting of water, methanol, ethanol, isopropanol, acetone and acetonitrile and combinations thereof. 
     
     
       5. A pharmaceutical composition comprising the crystalline form A of mesaconine according to  claim 1 , and pharmaceutically acceptable excipients. 
     
     
       6. A method for treating heart failure in a subject, comprising administering thereto an effective amount of a crystalline form A of mesaconine according to  claim 1 , or a pharmaceutical composition comprising the crystalline form A of mesaconine and pharmaceutically acceptable excipients.

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